Benzothiophene, a sulfur-containing heterocycle, plays a crucial role in pharmaceutical and biological research due to its low toxicity, high solubility, and bioavailability. This aromatic structure, comprising a six-membered ring fused with a thiophene moiety, serves as a key scaffold for synthesizing biologically significant compounds. Benzothiophene derivatives exhibit diverse biological and pharmacological activities, including antimicrobial, anticancer, anti-inflammatory, antioxidant, antimalarial, antidiabetic, and enzyme-inhibiting properties. This study utilizes the synthesis of Schiff base ligands with the benzothiophene moiety to build coordination complexes with metals. The electron-rich sulfur and aromaticity of the benzo[b]thiophene core are well-known for their ability to stabilise the metal centres and have an impact on the coordination compounds' overall shape and reactivity. This review focuses on the advancements in the biological activities of benzothiophene compounds, emphasizing their potential as Schiff base metal complexes with enzyme-inhibiting capabilities. The discussion aims to provide new insights into the development of safer and more effective benzothiophene-based medicinal drugs, analytical agents, and pathological probes.